BBO-10203 是一种强效的 PI3Kα 和 KRASG12C 抑制剂，选择性地并与 RAS 结合域中的 Cys242 共价结合，抑制 KRASG12C 的 GTP 结合状态和 GDP 结合状态，其 IC50 为 0.031 nM，EC50 为 0.02 nM。BBO-10203 扰乱了 RAS 各异构体与 PI3Kα 之间的相互作用，导致 RAS 介导的 PI3Kα 激活被抑制，并降低 pERK 表达，细胞增殖，诱导 G1 期阻滞和凋亡 (apoptosis)。BBO-10203 可用于 乳腺癌、结直肠癌 和 非小细胞肺癌 的研究。
| 生物活性 |
BBO-10203 is a potent inhibitor of PI3Kα and KRASG12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer. |
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| 分子式 |
C34H30F2N6O3S
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| 分子量 |
640.70
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| CAS号 |
2971769-60-3
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
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纯度： 98%
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400-881-9290
Data Sheet
